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Use of stabilized granules containing glyceryl trinitrate for arteriogenesis

a technology of glyceryl trinitrate and stabilized granules, which is applied in the directions of pharmaceutical delivery mechanisms, organic active ingredients, and heterocyclic compound active ingredients, can solve the problems that nitroglycerin has not been used for curing the underlying disease or improving the prognosis, so as to reduce volatility

Active Publication Date: 2016-02-02
G POHL BOSKAMP GMBH & CO KG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0011]In a first aspect, the present invention relates to a method of treating or preventing an arterial insufficiency, wherein an NO donor is administered in an intermitting manner to a subject in an amount effective for the induction of arteriogenesis, and wherein the NO donor is glyceryl trinitrate in a solid pharmaceutical preparation for oromucosal or oral administration characterized in that it contains between 0.05 and 2 weight % glyceryl trinitrate (GTN), at least one diluent, one carrier material, and at least one substance that reduces the volatility of GTN, whereby this substance is a non-volatile ester stabilizer whose melting point is not higher than 60° C.

Problems solved by technology

However, nitroglycerin has not been used for curing the underlying disease or improving its prognosis.

Method used

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  • Use of stabilized granules containing glyceryl trinitrate for arteriogenesis
  • Use of stabilized granules containing glyceryl trinitrate for arteriogenesis
  • Use of stabilized granules containing glyceryl trinitrate for arteriogenesis

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0228]

ContentsQuantity [g]GTN (5%) in diluent MCT1.033Triethyl citrate1.032Isomalt16.513Xylitol6.248Silicon dioxide (Aeroperl ®)0.207Total25.033GTN concentration0.207%

[0229]Triethyl citrate was mixed with GTN phlegmatized in a diluent of medium chain triglycerides (MCT). The solution was mixed well with the isomalt. Then xylitol and finally silicon dioxide were added and mixing was continued. 200-mg portions of the free-flowing powder were filled in stick packs and stored at 40° C. / 75% rel humidity for three months.

[0230]The GTN concentration was quantified after production and at various points during storage using HPLC analysis. The individual doses were dissolved in a suitable solvent to perform the analysis. The GTN was detected using a UV-VIS detector at a wavelength of 225 nm.

[0231]

GTN concentration following storage at 40° C. / 75% rel. humidityProductaccording to0 months2 weeks1 month3 monthsComp.0.391 mg0.079 mg0.065 mg*example 1Comp.0.407 mgn.c.0.305 mg0.245 mgexample 2Examp...

example 2

[0233]

ContentsQuantity [g]GTN (5%) in diluent MCT2.00TPGS1.00Magnesium aluminometasilicate2.50Isomalt44.5Total50.00GTN concentration0.20%

[0234]TPGS was melted at 50° C. and mixed with GTN concentrate in a diluent of MCT. While still warm, the mixture was blended well with the magnesium aluminometasilicate. Then isomalt was added and mixing was continued. 200-mg portions of the free-flowing powder were filled in stick packs and stored at 25° C. / 60% rel. humidity. The GTN concentration was quantified immediately after production and at various points during storage as disclosed under Example 1. The results are presented in the following table:

[0235]

Storage duration / temp.0 months3 months / 25° C.6 months / 25° C.GTN concentration0.400 mg0.398 mg0.392 mg

example 3

[0236]

ContentsQuantity [g]GTN (5%) in diluent MCT2.02Glycerol monocaprylocaprate Ph. Eur.0.52Magnesium aluminometasilicate1.50Isomalt45.99Total50.03GTN concentration0.20%

[0237]The glycerol monocaprylocaprate was melted at 40° C. and mixed with a GTN concentrate in MCT diluent. While still warm, the mixture was blended well with the magnesium aluminometasilicate. Then isomalt was added and mixing was continued. 200-mg portions of the free-flowing powder were filled in stick packs and stored at 40° C. / 75% rel humidity and at 25° C. / 60% rel. humidity. The GTN concentration was quantified immediately after production and at various points during storage as disclosed under Example 1. The results are presented in the following table:

[0238]

Storage duration / temp.0 months6 months / 25° C.6 months / 40° C.GTN concentration0.397 mg0.383 mg0.355 mg

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Abstract

The present invention inter alia relates to a method of treating or preventing an arterial insufficiency, wherein an NO donor is administered in an intermitting manner to a subject in an amount effective for the induction of arteriogenesis, and wherein the NO donor is a solid pharmaceutical preparation with the active substance glyceryl trinitrate for oromucosal or oral administration characterized in that it contains between 0.05 and 2 weight % glyceryl trinitrate (GTN), at least one diluent, one carrier material, and at least one substance that reduces the volatility of GTN, whereby this substance is a non-volatile ester stabilizer whose melting point is not higher than 60° C.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit under 35 U.S.C. §119(e) to U.S. Provisional Application No. 61 / 653,601, filed May 31, 2012, the entire disclosure of which is hereby incorporated herein by reference for all purposes.FIELD OF INVENTION[0002]The present invention relates to methods of treating or preventing an arterial insufficiency by the administration of a NO (nitric oxide) donor.BACKGROUND[0003]Cardiovascular diseases as well as other diseases involving a cardiovascular and, more specifically, arterial insufficiency have an enormous economic importance. In Germany, for example, about 280000 patients suffer every year from a cardiac infarct, while about 65000 patients die. One important reason for a cardiovascular disease is the partial or complete occlusion of arterial vessels resulting in a reduced supply of oxygen and nutrients of the tissue supplied by the arterial vessel.[0004]Angina pectoris, the chest pain, is a clinical syndro...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K31/21A61K9/14A61K31/34A61K31/616A61K9/16A61K9/00
CPCA61K9/14A61K9/006A61K9/145A61K9/1617A61K9/1623A61K31/21A61K31/34A61K31/616A61K2300/00A61K9/1611
Inventor GORATH, MICHAELA
Owner G POHL BOSKAMP GMBH & CO KG
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